Home : DrugWatch : Prinivil : Wikipedia : Lisinopril

Wikipedia - Lisinopril
This article has multiple issues. Please help improve the article or discuss these issues on the talk page.
Lisinopril
Systematic (IUPAC) name
N2-[(1S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline
Identifiers
CAS number 83915-83-7
ATC code C09AA03
PubChem CID 5362119
DrugBank APRD00560
ChemSpider 4514933
Chemical data
Formula C21H31N3O5 
Mol. mass 405.488 g/mol
SMILES eMolecules & PubChem
Synonyms (2S)-1-[(2S)-6-amino-2-{[(1S)-1-carboxy-3-phenylpropyl]amino}hexanoyl]pyrrolidine-2-carboxylic acid
Pharmacokinetic data
Bioavailability approx. 25%, but wide range between individuals (6 to 60%)
Protein binding 0
Metabolism None
Half-life 12 hours
Excretion Eliminated unchanged in Urine
Therapeutic considerations
Pregnancy cat. D - teratogenic
Legal status ? Prescription only
Routes PO

Lisinopril (lye-SIN-o-pril) is a drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in treatment of hypertension, congestive heart failure, heart attacks and also in preventing renal and retinal complications of diabetes. It has been compared with omapatrilat which is of similar function.

Historically, lisinopril was the third ACE inhibitor, after captopril and enalapril, and was introduced into therapy in the early 1990s.[1] Lisinopril has a number of properties that distinguish it from other ACE inhibitors: it is hydrophilic, has long half-life and tissue penetration and is not metabolized by the liver.

Lisinopril was developed by Merck & Co. and is marketed worldwide as Prinivil or Tensopril and by AstraZeneca as Zestril. In India it is marketed by Micro Labs as Hipril. In the United States, a generic version is available. Like other ACE inhibitors, it is derived from the venom of the jararaca, a Brazilian pit viper (Bothrops jararaca)[2]. Lisinopril can also be used in conjunction with the diuretic Hydrochlorothiazide and drugs which combine these two medications are available under the brand names Prinzide and Zestoretic.

Contents

[edit] Pharmacology

Lisinopril is the lysine-analog of enalapril. Unlike other ACE inhibitors, lisinopril is not a prodrug and is excreted unchanged in the urine. In cases of overdosage, it can be removed from circulation by dialysis.

[edit] Pharmacokinetics and metabolism

Adult patients: Following oral administration of lisinopril, peak serum concentrations occur within about 7 hours, although there was a trend to a small delay in time taken to reach peak serum concentrations in acute myocardial infarction patients. Declining serum concentrations exhibit a prolonged terminal phase which does not contribute to drug accumulation. This terminal phase probably represents saturable binding to ACE and is not proportional to dose. Lisinopril does not appear to be bound to other serum proteins.

Lisinopril does not undergo metabolism and is excreted unchanged entirely in the urine. Based on urinary recovery, the mean extent of absorption of lisinopril is approximately 25 percent, with large inter-subject variability (6-60 percent) at all doses tested (5-80 mg). Lisinopril absorption is not influenced by the presence of food in the gastrointestinal tract. The absolute bioavailability of lisinopril is reduced to about 16 percent in patients with stable NYHA Class II-IV congestive heart failure, and the volume of distribution appears to be slightly smaller than that in normal subjects.

The oral bioavailability of lisinopril in patients with acute myocardial infarction is similar to that in healthy volunteers.

Upon multiple dosing, lisinopril exhibits an effective half-life of accumulation of 12 hours.

Impaired renal function decreases elimination of lisinopril, which is excreted principally through the kidneys, but this decrease becomes clinically important only when the glomerular filtration rate is below 30 mL/min. Above this glomerular filtration rate, the elimination half-life is little changed. With greater impairment, however, peak and trough lisinopril levels increase, time to peak concentration increases and time to attain steady state is prolonged. Older patients, on average, have (approximately doubled) higher blood levels and area under the plasma concentration time curve (AUC) than younger patients.

[edit] Clinical use

Its indications, contraindications and side effects are as those for all ACE inhibitors. Its long half-life allows for once a day dosing which aids patient compliance. The usual daily dose in all indications ranges from 2.5 mg/day in sensitive patients to 20 mg/day in more tolerant or unresponsive subjects. [3] Some patients have been treated with 80 mg daily and have tolerated this high dose well. Lower dosages must be used in patients with higher grade renal impairment (glomerular filtration rate (GFR) lower than 30 ml/min).

Patients whose creatinine clearance =10 mL/min and =30 mL/min (typically with a serum creatinine =3 mg/dL) should be given the standard 5 mg/day dosage, at first.[4] For patients whose creatinine clearance is less than 10 mL/min, the dosage should start at 2.5 mg/day, adjusted over time according to the patient's blood pressure response.

[edit] Adverse effects

Side effects, some or all of which are serious and require immediate medical attention, include:

  • Chills, infection
  • Dark urine, decreased urination (oliguria)
  • Difficulty swallowing or breathing (signs of angioedema), allergic reaction (anaphylaxis)
  • Hoarseness
  • Itching
  • Rapid weight gain, stomach pain
  • Yellowing of skin or eyes (jaundice)
  • Abdominal pain, bloating, vomiting
  • Chest pain or tightness, dizziness, lightheadedness, fainting (syncope)
  • Dry cough
  • Fever
  • Joint pain
  • Rash
  • Diarrhea, loss of taste, nausea
  • Drowsiness, headache, tiredness
  • Change in mood/irrational behaviour
  • Blurred vision
  • Muscle cramps
  • Fainting/blackouts
  • Sexual dysfunction
  • Serious (possibly fatal) liver problems[5]

Lisinopril causes the kidneys to retain potassium, which may lead to hyperkalemia.

A rare but severe allergic reaction can occur that affects the bowel wall and secondarily causes abdominal pain. This "anaphylactic" reaction is very rare, and must be given immediate medical attention.

[edit] See also

[edit] References

  • Bussien JP, Waeber B, Nussberger J, Gomez HJ, Brunner HR. Once-daily lisinopril in hypertensive patients: Effect on blood pressure and the renin-angiotensin system. Curr Therap Res 1985;37:342-51.
  • Lisinopril info - rx-list.com
  • Goodman & Gilman's : The pharmacological basis of therapeutics, 10th. ed., 2001
  • Lisinopril.com - Lisinopril information

[edit] Footnotes

  1. ^ Patchett A, Harris E, Tristram E, Wyvratt M, Wu M, Taub D, Peterson E, Ikeler T, ten Broeke J, Payne L, Ondeyka D, Thorsett E, Greenlee W, Lohr N, Hoffsommer R, Joshua H, Ruyle W, Rothrock J, Aster S, Maycock A, Robinson F, Hirschmann R, Sweet C, Ulm E, Gross D, Vassil T, Stone C (1980). "A new class of angiotensin-converting enzyme inhibitors". Nature 288 (5788): 280–3. doi:10.1038/288280a0. PMID 6253826. 
  2. ^ Patlak M. 2004. "From Viper's Venom to Drug Design: Treating Hypertension". The FASEB Journal. 18, no. 3.
  3. ^ "Lisinopril Dosage, Interactions, Side Effects, How to Use". Health Digest, Retrieved 27 May 2010.
  4. ^ "Lisinopril Dosage, Interactions, Side Effects, How to Use" Health Digest, Retrieved 27 May 2010.
  5. ^ "Lisinopril Oral : Uses, Side Effects, Interactions, Pictures, Warnings & Dosing". WebMD. http://www.webmd.com/drugs/drug-6873-Lisinopril+Oral.aspx?drugid=6873&drugname=Lisinopril+Oral&source=2. Retrieved April 20, 2010. 

[edit] External links

Stub icon This antihypertensive-related article is a stub. You can help Wikipedia by expanding it.
v • d • e
Antihypertensives: agents acting on the renin-angiotensin system (C09)
ACE inhibitors
("-pril")
AIIRAs/
("-sartan")
Renin inhibitors/
("-kiren")
Retrieved from "http://en.wikipedia.org/wiki/Lisinopril"

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Lisinopril".

Need A Prinivil Attorney?

First Name Last Name Email Address State
Has Your Health Been Negatively Affected?

Please Describe the Injury

Your Friend's Email Address

Your Email Address

Type a Message (optional)


Want to contact a Washington, DC Prinivil attorney? ...Get a free case evaluation from one of our Washington, DC Prinivil attorneys now.

 

Close (x)

Looking for an Attorney?


Please type your question:

Close (x)

logo Find Legal Help for Your Prinivil Case - Submit Your Information Below

Do you need legal assistance with your Prinivil case?
LegalView may be able to help.


Submit your information below for a free, no-cost evaluation.

We'll submit your information to one of our partner firms.
LegalView's partners represent clients throughout the United States, for a very wide range of legal issues. Submit your information now, to see if one of LegalView's partners can help!

* Indicates Required Fields

First name *
Last name *
Email Address *
Phone Number *
()  -

State *
Legal Issue * DrugWatch: Prinivil Change
Was There an Injury?
Please Describe The Injury

DISCLAIMER and STATEMENT OF NON-CONFIDENTIALITY

By submitting this form, you agree that completing the above is not intended to create an attorney-client relationship.

Disclosure

Legal WebTV Network LLC, LegalView.com, and LegalWebMedia.com are group advertising sponsored by the attorneys identified here. It is not a lawyer referral service. If you submit information on this website [more...]

Legal WebTV Network LLC, LegalView.com, and LegalWebMedia.com are group advertising sponsored by the attorneys identified here. It is not a lawyer referral service. If you submit information on this website, LegalWebMedia.com will submit your information to the law firms that pay for this group advertising and to respond to your requests for information concerning legal services in their assigned local areas. If there is no sponsoring firm in your state, your inquiry will be submitted to one of the sponsoring law firms on a predetermined, rotating basis. If the sponsoring law firm accepts your case, it will associate with licensed attorneys practicing in your state, if required; the sponsoring law firm may also contact other law firms to see if they may be able to assist.

The information provided by the LegalView.com and LegalWebMedia.com websites is for advertising and informational purposes and should not be considered as legal advice from the sponsoring attorneys. The websites contain general information and may not reflect current legal developments, verdicts, or settlements. LegalView.com contains information created by others or supplied through open forums; the sponsoring law firms are not responsible for the accuracy of this information. Any person viewing or receiving information from these websites should not act or refrain from acting on the basis of any such information without first seeking appropriate legal advice from an attorney in your area. Legal WebTV Network, LLC expressly disclaims any liability with respect to actions taken or not taken by the recipient based on any or all of the information or contents contained in these websites.

Any information sent to Legal WebTV Network LLC through this website is done using standard Web encryption techology. LegalView.com will exercise all reasonable care, within technological limits, to protect the confidentiality of any information submitted via Internet e-mail or through this website. By accessing this website, you may be seeking an attorney to represent you or legal advice. However, none of the sponsoring attorneys represent you yet.

The choice of a lawyer is an important decision and should not be based solely upon advertisements.

Any transmission of information, whether via Internet e-mail or through the website, is solely for evaluation purposes by the sponsoring law firms and their associates. The transmission of any information to any attorney sponsoring advertising on LegalView.com or LegalWebMedia.com does not create an attorney-client relationship between the sender and any recipient. An attorney-client relationship can only be created by a written, signed-fee agreement entered into with an attorney. The sponsoring attorneys will treat your information as a confidential communication for the purpose of obtaining legal services or legal advice.

For more information about the sponsoring law firms, please click here.
This form is secure and encrypted. More information about secure forms and your privacy here.